A growth hormone engineered to block its own receptor, and what it showed about the mechanism

Published 26 October 2026 · REVIVE LAB UAE Research Desk · 5 min read
Pegvisomant is a 191-residue growth hormone variant with glycine 120 replaced by lysine, which abolishes binding at site 2, and eight further substitutions at site 1 that raise its affinity there, with polyethylene glycol chains attached to extend its half-life. It binds one receptor molecule tightly and cannot recruit the second, so no signal follows and the native hormone is excluded. Trainer and colleagues reported in the New England Journal of Medicine in 2000 that it normalised IGF-1 in most patients with acromegaly, and it was approved in 2003. It is the direct therapeutic proof of the two-site model.

How it was designed

The alanine-scanning and crystal-structure work of 1989 to 1992 located the two receptor-binding sites and identified glycine 120 as a residue at site 2 whose replacement with a bulky side chain prevented the second receptor from binding. Phage display then selected site 1 mutations that increased affinity. The engineered protein, called B2036 before pegylation, bound the receptor better than the natural hormone and did nothing.

Pegylation lowered its affinity somewhat but extended its circulation from minutes to days.

What the 2000 trial showed

In 112 patients with acromegaly, IGF-1 fell into the normal range in the great majority of those receiving the active drug over twelve weeks, with symptom improvement. Growth hormone itself rose, because the feedback that normally restrains it was blocked, which is why treatment is monitored by IGF-1 rather than growth hormone.

It remains the only growth hormone receptor antagonist in clinical use.

What it establishes

That receptor activation requires both sites and that blocking one is enough to abolish signalling in vivo. It is pharmacology of the receptor, stated here because the receptor is what the hormone in the pack acts on.

Somatropin is supplied by REVIVE LAB UAE for laboratory research use only, with identity and purity documented for the batch. It is not for human or veterinary use, and no dosing, administration or protocol guidance is provided.

What it costs

FormatStrengthPriceAvailability
HGH Somatropin Pack24 mg (72 IU)AED 850In stock

Delivery is AED 40 flat and free on orders over AED 700. Payment is cash on delivery anywhere in the UAE, or USDT (TRC20) in advance, which takes 5% off the order total.

Frequently asked

How it was designed?

The alanine-scanning and crystal-structure work of 1989 to 1992 located the two receptor-binding sites and identified glycine 120 as a residue at site 2 whose replacement with a bulky side chain prevented the second receptor from binding. Phage display then selected site 1 mutations that increased affinity. The engineered protein, called B2036 before pegylation, bound the receptor better than the natural hormone and did nothing.

Does REVIVE LAB UAE provide dosing guidance?

No. REVIVE LAB UAE supplies research materials and provides no dosing, administration or protocol guidance of any kind. Every product is sold for laboratory research use only and is not for human or veterinary consumption.

How fast is delivery in the UAE?

Stock is held in Dubai. An order confirmed before 4 PM Dubai time is dispatched the same working day, reaching Dubai and Abu Dhabi the same day and the remaining emirates within 24 hours. Delivery is AED 40 flat and free over AED 700.

HGH Somatropin Pack — in stock, dispatched from Dubai
HPLC-verified, lot certificate on every carton, 24-hour delivery nationwide. Browse the catalogue → All peptides UAE

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Supplied for laboratory research use only. Not for human or veterinary consumption. REVIVE LAB UAE provides no dosing, administration or protocol guidance.